( 1) Field of Invention
1-Substituted-4-aroyl-4-hydroxy and -4-acyloxypiperidines and acid addition salts thereof; central nervous system depressant, neuroleptic compounds; compositions thereof; method of treating therewith; production thereof; intermediates therefor.
( 2) Prior Art
A number of ketones of the general formula ##STR1## wherein R.sub.3 and R.sub.4 are widely different groups, have been made and tested. As to these type compounds, Janssen (Cavallito, "Structure-Activity Relationships I", page 37) has stated that one of the groups R.sub.3 and R.sub.4 must be aromatic and that only one may be hydrogen if the ketone is to be an anti-psychotic.
Three clinically-established compounds in this field are as follows, namely:
Haloperidol, of the foregoing formula, wherein R.sub.3 = OH and R.sub.4 = ##STR2##
Chlorpromazine, having the formula ##STR3## and Pimozide, having the formula ##STR4##
These established clinically-useful compounds of the prior art have, however, been found to be characterized by pronounced shortcomings and side-effects, and there is a clear demand for more specific and advantageous compounds in this activity and utility area, especially central nervous system depressants and neuroleptics with pronounced antipsychotic effect. The fulfillment of this demand is one of the objects of the present invention, as will become more fully apparent hereinafter.